Lead Optimization

This course covers the stages of drug discovery in which promising compounds (leads) are identified, their optimal and suboptimal characteristics determined, and the suboptimal characteristics optimized to create a candidate suitable for the clinic.  The course is built around a case study on the discovery of an antimalarial therapy.  [...]

Understanding the efficacy, potency, pharmacokinetics, and safety of compounds is important, but compounds almost always require improvement in their properties in order to become drugs. The process of improvement is called lead optimization and requires a thorough understanding of how a molecule’s structure affects its function, whether efficacy, PK, [...]

Once a person understands the ideas of drug efficacy, potency, pharmacokinetics, and safety, original research articles can be readily understood. The Journal of Medicinal Chemistry of the American Chemical Society regularly publishes a series of articles called Drug Annotations. These articles summaries a drug discovery program from a pharmaceutical [...]